Depression is the most common psychiatric disease against human health. By far 3-5% of the population of the world suffers from depression. It is expected by 2020 depression might be the major disease second to heart disease.
Medicines are commonly used to treat depression and comprise tricyclic antidepressant agent like imipramine etc.; monoamine oxidase inhibitor like moclobemide etc.; selective 5-HT reuptake inhibitor like fluoxetine etc.; selective NE reuptake inhibitor like reboxetine etc.; 5-HT and NE double reuptake inhibitor like duloxetine etc.
Although various antidepressant agents have been clinically used, some medicines have the disadvantages of low response rate, long onset time and potential adverse effect and thus a large number of patients are ineffective to various therapies and some of them even turn to electrofit therapy. Accordingly, it is desirable to develop novel antidepressant agent.
U.S. Pat. No. 4,018,895 discloses antidepressant agents including fluoxetine having the following structure:
wherein, Ar is naphthalene ring or substituted benzene ring, R1 and R2 are each H or methyl.
CN 1019113 discloses antidepressant agents including duloxetine having the following structure:
wherein, Ar is naphthalene ring or substituted benzene ring; Ar1 is cycloalkyl, furyl, thienyl or thiazolyl; R1 and R2 are each H or CH3.
CN 101613347 discloses antidepressant compounds including ammuxetine having the following structure:
wherein X is O or S, R1 and R2 each independently represent H or C1-C3 alkyl.
Although the above medicines like duloxetine and ammuxetine have relatively good activity against depression, their structures are not stable against acid, are prone to decomposition in stomach, not suitable for disintegration and uptake in stomach and thus are not suitable for preparing normal tablet and have high selectivity for formulation.